General Information of Drug (ID: DMWZ2TU)

Drug Name
CO-1686 Drug Info
Synonyms
1374640-70-6; AVL-301; CO1686; UNII-72AH61702G; CNX-419; CO-1686 (AVL-301); Rociletinib(AVL-301,CNX-419,CO-1686); 72AH61702G; N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide; CO 1686; Rociletinib (CO-1686, AVL-301); Rociletinib [USAN:INN]; Tube721; Rociletinib (USAN/INN); Rociletinib (CO-1686); SCHEMBL4177736; GTPL7966; CHEMBL3545308; EX-A228; MolPort-035-395-816; C27H28F3N7O3; HMS3653G08; BDBM149404; BCP07085; AOB87314; ZINC98043800; s7284
Indication
Disease Entry ICD 11 Status REF
Lung cancer 2C25.0 Phase 3 [1]
Non-small-cell lung cancer 2C25.Y Phase 3 [2]
Cross-matching ID
PubChem CID
57335384
CAS Number
CAS 1374640-70-6
TTD Drug ID
DMWZ2TU

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [5]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [6]
Gefitinib DM15F0X Colon adenocarcinoma Approved [7]
Erlotinib DMCMBHA Adrenal gland neoplasm Approved [8]
Vandetanib DMRICNP Solid tumour/cancer 2A00-2F9Z Approved [9]
Dacomitinib DMOH8VY Non-small-cell lung cancer 2C25.Y Approved [10]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [11]
SKI-758 DMQ8E9R Ischemia 8B10-8B11 Approved [12]
Epidermal growth factor DMVONE6 Vulnerary ND56.Z Approved [10]
Merimepodib DM0HS92 Breast cancer 2C60-2C65 Approved [13]
BIBW 2992 DMTKD7Q Non-small-cell lung cancer 2C25.Y Approved [14]
Gefitinib DM15F0X Colon adenocarcinoma Approved [15]
Erlotinib DMCMBHA Adrenal gland neoplasm Approved [16]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [17]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [18]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [19]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [20]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [21]
Selenium DM25CGV N. A. N. A. Approved [22]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [23]
⏷ Show the Full List of 20 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Modulator [3]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Epidermal growth factor receptor (EGFR) OTAPLO1S EGFR_HUMAN Gene/Protein Processing [4]

References

1 ClinicalTrials.gov (NCT02322281) TIGER-3: Open Label, Multicenter Study of Rociletinib (CO-1686) Mono Therapy Versus Single-agent Cytotoxic Chemotherapy in Patients With Mutant EGFR NSCLC Who Have Failed at Least One Previous EGFR-Directed TKI and Platinum-doublet Chemotherapy
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7966).
3 Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1700-9.
4 Osimertinib induces autophagy and apoptosis via reactive oxygen species generation in non-small cell lung cancer cells. Toxicol Appl Pharmacol. 2017 Apr 15;321:18-26. doi: 10.1016/j.taap.2017.02.017. Epub 2017 Feb 22.
5 Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
6 Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
7 Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
8 Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
9 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
10 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1797).
11 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
12 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
13 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
14 Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. J Med Chem. 2011 Mar 10;54(5):1347-55. doi: 10.1021/jm101396q. Epub 2011 Feb 15.
15 Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
16 Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med. 2004 May 20;350(21):2129-39. doi: 10.1056/NEJMoa040938. Epub 2004 Apr 29.
17 The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
18 A fine-needle aspirate-based vulnerability assay identifies polo-like kinase 1 as a mediator of gemcitabine resistance in pancreatic cancer. Mol Cancer Ther. 2010 Feb;9(2):311-8. doi: 10.1158/1535-7163.MCT-09-0693. Epub 2010 Jan 26.
19 Prediction of chemosensitivity using multigene analysis in head and neck squamous cell carcinoma. Oncology. 2007;73(1-2):104-11. doi: 10.1159/000120998. Epub 2008 Mar 13.
20 Sertraline induces endoplasmic reticulum stress in hepatic cells. Toxicology. 2014 Aug 1;322:78-88. doi: 10.1016/j.tox.2014.05.007. Epub 2014 May 24.
21 Minimal peroxide exposure of neuronal cells induces multifaceted adaptive responses. PLoS One. 2010 Dec 17;5(12):e14352. doi: 10.1371/journal.pone.0014352.
22 Inhibition of invasion and induction of apoptosis by selenium in human malignant brain tumour cells in vitro. Int J Oncol. 2007 May;30(5):1263-71.
23 Ligand-dependent activation of the epidermal growth factor receptor by secondary bile acids in polarizing colon cancer cells. Surgery. 2005 Sep;138(3):415-21. doi: 10.1016/j.surg.2005.06.030.